NCI172112 (NSC172112)
(Synonyms: 螺莫司汀,NSC172112; NSC268497) 目录号 : GC34194
NCI172112 (NSC172112) 是一种经典的双功能烷化剂，旨在开发对 CNS 肿瘤有效的抗肿瘤剂。
Cas No.:56605-16-4
Sample solution is provided at 25 µL, 10mM.
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NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
NCI172112 (Spirohydantoin mustard, SHM) might serve as a carrier to cross the blood brain barrier[1]. The cumulative excretion of radioactivity in the urine and faeces of rats after administration of [2-chloroethyl-U-14C]NCI172112 or [hydantoin-4-14C]NCI172112 ( 3.13 mg/kg. i.v.) is measured. Four hours after dosing, a significantly (P<0.005) greater amount of radioactivity has been excreted in the urine of rats treated with [hydantoin-14C]NCI172112 than with [ethyl-14C]NCI172112. However, by 24 h, approx.50% of dose is recovered in the urine with both labelled materials. Clearance of radioactivity in the faeces is slow, but, as for the renal excretion, is significantly greater for the hydantoin-14C moiety. No radioactivity is found in the expired air of a rat receiving a single dosing of [hydantoin-14C]NCI172112 and less than 1% is measured after administration of [ethyl-14C]NCI172112. Renal clearance of radioactivity is similar 4 h after administration of [14C]NCI172112 to rats with biliary cannulas, with 14.1±2.9 and 17.5±2.1% of the ethyl-14C and 34.5±2.5 and 33.1±6.3%, of the hydantoin-14C dose appearing in the urine after dosing with 3.13 and 6.25 mg/kg,respectively. A difference in the 4 h urinary excretion of the two labels also is observed in dogs given [14C]NCI172112 (1 mg/kg, i.v.). The percentages of hydantoin-14C and ethyl-14C eliminated are 29.4±2.7% and 17.2±3.5%, respectively (P<0.05)[2].
[1]. Brown TD, et al. A phase I trial of spirohydantoin mustard (NSC 172112) in patients with advanced cancer. J Clin Oncol. 1986 Aug;4(8):1270-6. [2]. Plowman J, et al. The disposition of spirohydantoin mustard (NSC 172112) in rats and dogs. Xenobiotica. 1979 Jun;9(6):379-91.
Animal experiment: | Rats[2]Male Sprague-Dawley rats (190-240 g) are lightly anaesthetized with pentobarbital (30 mg/kg i.p.) and [14C]NCI172112 (2 μCi/rat, 3.13 mg/kg) dissolved in DMSO injected into the femoral vein. The animals are individually housed in glass metabolic cages, with access to food and water for 96 h, and urine and faeces are collected separately. At 96 h, the rats are killed with an overdose of pentobarbital and each carcass is homogenized in 4 vol. water with a Waring blender. Radioactivity in aliquots of drug soln. and urine are measured by liquid scintillation counting with 15 mL phosphor.Dogs[2]Female foxhounds, weighing 15-20 kg, are anaesthetized with pentobarbital (30 mg/kg) and are maintained in this state throughout the experiment with aditional pentobarbital. [14C] NCI172112 (50-60 μCi, 1 mg/kg) in 1 mL DMSO is administered to the dogs via a catheter inserted into the femoral vein. Blood samples are withdrawn from the femoral artery by means of an indwelling catheter at timed intervals from 1 min to 4 h and transferred to heparinized tubes chilled on crushed ice. Immediately, a 0.5 mL aliquot is removed and extracted with three 2 mL vol. of cold toluene. The remaining blood is centrifuged, and 0.5 mL aliquots of plasma digested with NCS, extracted with 2 mL vol. of toluene or diluted with 2 mL 10% trichloroacetic acid. From the initial sampling of the dog blood to the start of the extraction or pptn. procedures for plasma, 8-14 min elapsed. |
References: [1]. Brown TD, et al. A phase I trial of spirohydantoin mustard (NSC 172112) in patients with advanced cancer. J Clin Oncol. 1986 Aug;4(8):1270-6. | |
| Cas No. | 56605-16-4 | SDF | |
| 别名 | 螺莫司汀,NSC172112; NSC268497 | ||
| Canonical SMILES | O=C(N1CCN(CCCl)CCCl)NC2(CCCCC2)C1=O | ||
| 分子式 | C14H23Cl2N3O2 | 分子量 | 336.26 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9739 mL | 14.8694 mL | 29.7389 mL |
| 5 mM | 0.5948 mL | 2.9739 mL | 5.9478 mL |
| 10 mM | 0.2974 mL | 1.4869 mL | 2.9739 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
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